EMAIL THIS PAGE TO A FRIEND
BM0033 Sigma

BMS-665053

≥98% (HPLC)

Synonym: (S)-5-Chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(difluoromethoxy)phenylamino)-pyrazin-2(1H)-one, 5-Chloro-1-[(1S)-1-cyclopropylethyl]-3-[[2,6-dichloro-4-(difluoromethoxy)phenyl]amino]-2(1H)-pyrazinone

  • CAS Number 1173435-64-7

  • Empirical Formula (Hill Notation) C16H14Cl3F2N3O2

  • Molecular Weight 424.66

  •  MDL number MFCD28977961

Purchase

Properties

Related Categories B, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience,
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D +16 to +21°, c = 0.4 in chloroform-d
color   white to light brown
solubility   DMSO: 20 mg/mL, clear
storage temp.   room temp

Description

Packaging

5, 25 mg in glass bottle

Legal Information

Sold for research purposes only under agreement from BMS.

Biochem/physiol Actions

BMS-665053 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 </= 1.0 nM against 150 pM ovine CRF for binding human and rat CRF-R1), potency (IC50 = 4.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying no affinity toward CRF-R2/CRF2 (IC50 >10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%).

Features and Benefits

BMS-665053 is available through a partnership between Sigma Life Science and Bristol-Myers Squibb (BMS). To learn more and view other BMS compounds, visit sigma.com/BMS.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis

Protocols & Articles

Related Content

Discover Bristol-Myers Squibb Compounds

Sigma® Life Science understands that in your research, the right tools are essential. Our commitment to providing researchers with the broadest selection of reliable, quality-controlled tools has res...
Keywords: Bioactive small molecules, Clinical, Genomics, Immunology, Neuroscience, Research areas

Peer-Reviewed Papers
15

References

Related Products

Technical Service:

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Bulk Ordering & Pricing:

Need larger quantities for your development, manufacturing or research applications?


Discover your Target